Abstract:
:Elusive for more than half a century, corticotropin-releasing factor (CRF) was finally isolated and characterized in 1981 from ovine hypothalami and shortly thereafter, from rat brains. Thirty years later, much has been learned about the function and localization of CRF and related family members (Urocortins 1, 2 and 3) and their 2 receptors, CRF receptor type 1 (CRFR1) and CRF receptor type 2 (CRFR2). Here, we report the stepwise development of peptide CRF agonists and antagonists, which led to the CRFR1 agonist Stressin1; the long-acting antagonists Astressin2-B which is specific for CRFR2; and Astressin B, which binds to both CRFR1 and CRFR2.This analog has potential for the treatment of CRF-dependent diseases in the periphery, such as irritable bowel syndrome.
journal_name
Front Neuroendocrinoljournal_title
Frontiers in neuroendocrinologyauthors
Rivier JE,Rivier CLdoi
10.1016/j.yfrne.2013.10.006subject
Has Abstractpub_date
2014-04-01 00:00:00pages
161-70issue
2eissn
0091-3022issn
1095-6808pii
S0091-3022(13)00069-1journal_volume
35pub_type
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